Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, European Journal of Medicinal Chemistry called Synthesis and structure-activity relationship of furoquinolinediones as inhibitors of Tyrosyl-DNA phosphodiesterase 2 (TDP2), Author is Yu, Le-Mao; Hu, Zhu; Chen, Yu; Ravji, Azhar; Lopez, Sophia; Plescia, Caroline B.; Yu, Qian; Yang, Hui; Abdelmalak, Monica; Saha, Sourav; Agama, Keli; Kiselev, Evgeny; Marchand, Christophe; Pommier, Yves; An, Lin-Kun, which mentions a compound: 67914-60-7, SMILESS is CC(N1CCN(C2=CC=C(O)C=C2)CC1)=O, Molecular C12H16N2O2, Related Products of 67914-60-7.
Tyrosyl-DNA phosphodiesterase 2 (TDP2) is a recently discovered enzyme specifically repairing topoisomerase II (TOP2)-mediated DNA damage. It has been shown that inhibition of TDP2 synergize with TOP2 inhibitors. Herein, we report the discovery of the furoquinolinedione chemotype as a suitable skeleton for the development of selective TDP2 inhibitors. Compound 1 was identified as a TDP2 inhibitor as a result of screening our inhouse compound library for compounds selective for TDP2 vs. TDP1. Further SAR studies provide several selective TDP2 inhibitors at low-micromolar range. The most potent compound 74 shows inhibitory activity with IC50 of 1.9 and 2.1 μM against recombinant TDP2 and TDP2 in whole cell extracts (WCE), resp.
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Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem